Product Description

The gastrin-releasing peptide receptor (GRPR), currently designated as BB2, is a G protein-coupled receptor encoded by the GRPR gene in humans, with gastrin-releasing peptide as its endogenous ligand. This receptor is highly expressed in the pancreas and is also present in the stomach, adrenal cortex, and brain. It functions through G protein-mediated activation of the phosphatidylinositol-calcium second messenger system, leading to Akt phosphorylation. The receptor contributes to the regulation of food intake and plays a specific role in the perception and transmission of pruritic stimuli—facilitating itch signal transduction in the spinal cord and promoting scratching behavior, without involvement in pain perception.

ScreeningBio’s CHO-K1/Human BB2 β-Arrestin cell line is an ideal tool for studying GPCR/β-arrestin interactions. In this system, the GPCR C-terminus is fused to a smallBiT tag, and the β2-arrestin N-terminus is fused to a largeBiT tag. Upon receptor activation, GPCR/β-arrestin interaction brings the two fragments together to reconstitute an active NanoLuc enzyme, which can be quantified using the NanoBiT substrate. This cell line is designed to evaluate a compound’s ability to activate the β-arrestin signaling pathway.